Quercetin nanocrystals for bioavailability enhancement: impact of different functional stabilizers on in vitro / in vivo drug performances.

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  • Additional Information
    • Source:
      Publisher: Informa Healthcare Country of Publication: England NLM ID: 9610932 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1097-9867 (Electronic) Linking ISSN: 10837450 NLM ISO Abbreviation: Pharm Dev Technol Subsets: MEDLINE
    • Publication Information:
      Publication: London : Informa Healthcare
      Original Publication: Monticello, NY : Marcel Dekker, c1996-
    • Subject Terms:
      Quercetin*/pharmacokinetics ; Quercetin*/administration & dosage ; Quercetin*/chemistry ; Quercetin*/pharmacology ; Nanoparticles*/chemistry ; Biological Availability* ; Solubility*; Animals ; Administration, Oral ; Male ; Particle Size ; Rats, Sprague-Dawley ; Drug Liberation ; Rats ; Excipients/chemistry ; Poloxamer/chemistry ; Glycyrrhizic Acid/chemistry ; Glycyrrhizic Acid/pharmacokinetics ; Glycyrrhizic Acid/administration & dosage ; Vitamin E/chemistry ; Vitamin E/pharmacokinetics
    • Abstract:
      The purpose of this study was to investigate the impact of different functional stabilizers on in vitro/in vivo drug performances after oral administration of drug nanocrystals. Quercetin nanocrystals (QT-NCs) respectively stabilized by five types of functional stabilizers, including hydroxypropyl methyl cellulose E15 (HPMC E15), poloxamer 407 (P407), poloxamer 188 (P188), D-α-tocopherol polyethylene glycol succinate (TPGS), and glycyrrhizin acid (GL), were fabricated by wet media milling technique. The particle size, morphology, physical state, drug solubility, drug dissolution in vitro , and orally pharmacokinetic behaviors of all QT-NCs were investigated. All QT-NCs with similar particle size about 200 nm were obtained by controlling milling speed and milling time. No significant differences in particles shape and crystalline nature were found for QT-NCs stabilized by different functional stabilizers. But the solubility and dissolution of QT-NCs were significantly influenced by the different functional stabilizers. The AUC 0∼ t of all QT-NCs after oral administration was in the following order: QT-NCs/P188 ≈ QT-NCs/HPMC E15 > QT-NCs/GL > QT-NCs/P407 ≈ QT-NCs/TPGS, and the C max showed an order of QT-NCs/P407 > QT-NCs/P188 ≈ QT-NCs/GL > QT-NCs/HPMC E15 > QT-NCs/TPGS. Both of QT-NCs/P407 and QT-NCs/TPGS exhibited faster oral absorption with T max at 0.5 h and 0.83 h, respectively, while the other three QT-NCs (QT-NCs/P188, QT-NCs/GL and QT-NCs/HPMC E15) showed a relatively slow absorption with same T max at 5.33 h. The longest MRT 0∼ t (11.72 h) and t 1/2z (32.22 h) were observed for QT-NCs/HPMC E15. These results suggested that the different functional stabilizers could significantly influence on drug solubility, drug dissolution in vitro and orally pharmacokinetic behavior of QT-NCs, and it is possible to alter the drug dissolution in vitro , oral absorption and drug retention in vivo by changing the type of functional stabilizers in NCs preparation.
    • Contributed Indexing:
      Keywords: Drug nanocrystals; functional stabilizers; in vitro/in vivo drug performances; oral administration; quercetin
    • Accession Number:
      9IKM0I5T1E (Quercetin)
      0 (Excipients)
      106392-12-5 (Poloxamer)
      6FO62043WK (Glycyrrhizic Acid)
      O03S90U1F2 (tocophersolan)
      1406-18-4 (Vitamin E)
    • Publication Date:
      Date Created: 20240529 Date Completed: 20240727 Latest Revision: 20240727
    • Publication Date:
      20240728
    • Accession Number:
      10.1080/10837450.2024.2361654
    • Accession Number:
      38808380